1. The structure of a new cardenolide diglycoside and the biological activities of eleven cardenolide diglycosides from Nerium oleander.
- Author
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Zhao M, Bai L, Toki A, Hasegawa R, Sakai J, Hasegawa T, Ogura H, Kataoka T, Bai Y, Ando M, Hirose K, and Ando M
- Subjects
- Anti-Inflammatory Agents isolation & purification, Anti-Inflammatory Agents toxicity, Antineoplastic Agents, Phytogenic isolation & purification, Antineoplastic Agents, Phytogenic toxicity, Cardenolides isolation & purification, Cardenolides pharmacology, Cell Line, Tumor, Drug Resistance, Neoplasm drug effects, Female, Fluoresceins metabolism, Humans, Magnetic Resonance Spectroscopy, Molecular Conformation, Ovarian Neoplasms drug therapy, Anti-Inflammatory Agents chemistry, Antineoplastic Agents, Phytogenic chemistry, Cardenolides chemistry, Nerium chemistry
- Abstract
A new cardenolide diglycoside (1) was isolated from Nerium oleander together with ten known cardenolide diglycosides 2-11. The structure of compound 1 was established on the basis of their spectroscopic data. The in vitro anti-inflammatory activity of compounds 1-11 was examined on the basis of inhibitory activity against the induction of the intercellular adhesion molecule-1 (ICAM-1). Compounds 2-5 were active at an IC(50) value of less than 0.8 µM. The cytotoxicity of compounds 1-11 was evaluated against three human cell lines normal human fibroblast cells (WI-38), malignant tumor cells induced from WI-38 (VA-13), and human liver tumor cells (HepG2). Compound 3 was active toward VA-13 cells, and compounds 2-5 were active toward HepG2 cells at IC(50) values of less than 1.3 µM. The multidrug resistance (MDR)-reversal activity of compounds 1-11 was evaluated on the basis of the amount of calcein in MDR human ovarian cancer 2780AD cells in the presence of each compound. Compounds 1 and 8 showed moderate effects on calcein accumulation.
- Published
- 2011
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